| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| Other Sizes |
| Targets |
nAChR[1]
nAChR (nicotinic acetylcholine receptor), specifically neuronal-type nicotinic receptors. (+)-Sparteine acts as a competitive antagonist, binding reversibly to the acetylcholine binding site on the receptor. This prevents the opening of the ion channel and blocks neurotransmission at autonomic ganglia and neuromuscular junctions. |
|---|---|
| ln Vitro |
At membrane potentials of -50 mV to +30 mV, (+)-Sparteine(2 μM) (sulfate pentahydrate) decreases the ACh-induced current brought on by the activation of nicotinic ACh receptors (AChRs) in a voltage-independent manner; however, at higher negative membrane potentials, its blocking action increases.The amplitude of excitatory postsynaptic currents (EPSCs) and the time constant of the EPSC decay are decreased by (+)-sparteine (5 μM and 10 μM) (sulfate pentahydrate)[1].
In vitro, (+)-Sparteine (2 microM) reduces the amplitude of nicotinic currents. It competitively blocks nAChR in neurons. The compound serves as a pharmacological tool to differentiate nicotinic responses from muscarinic responses in autonomic nervous system studies. It does not inhibit acetylcholinesterase. |
| ln Vivo |
In vivo, administration of (+)-Sparteine leads to ganglionic blockade, causing a fall in blood pressure (hypotension) due to reduced sympathetic tone. It was formerly used in obstetrics to shorten the first stage of labor. It has antiarrhythmic properties via effects on cardiac sodium channels (Class Ia antiarrhythmic) but is no longer commonly used.
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| Enzyme Assay |
A classic two-electrode voltage-clamp (TEVC) assay using Xenopus laevis oocytes expressing neuronal nAChR subunits (alpha3beta4 or alpha4beta2) is used. Oocytes are superfused with buffer containing ACh or nicotine in the absence or presence of (+)-Sparteine (0.1-100 microM). The reduction in peak ACh-evoked current is measured to determine IC50.
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| Cell Assay |
SH-SY5Y neuroblastoma cells expressing native nAChRs or HEK293 cells transfected with specific nAChR subunits are loaded with a calcium-sensitive dye (e.g., Fluo-4 AM). Cells are stimulated with a nicotinic agonist (e.g., 100 microM nicotine or DMPP) in the presence or absence of (+)-Sparteine. The reduction in intracellular calcium flux is measured by fluorescence plate reader.
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| Animal Protocol |
Male Sprague-Dawley rats or mice (C57BL/6) are anesthetized and the carotid artery is cannulated for blood pressure measurement. (+)-Sparteine (1-10 mg/kg) is administered intravenously, and the mean arterial pressure (MAP) is recorded continuously. A drop in MAP indicates successful ganglionic blockade. Heart rate is also monitored via ECG.
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| ADME/Pharmacokinetics |
In humans, (+)-Sparteine was administered intravenously (doses ranged from 50-150 mg) or intramuscularly. It is metabolized in the liver (cytochrome P450 2D6 is primarily responsible for sparteine oxidation). Sparteine exhibits polymorphic metabolism, leading to significant inter-individual variability in PK. The half-life is approximately 1-2 hours in extensive metabolizers but much longer in poor metabolizers.
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| Toxicity/Toxicokinetics |
Historically, toxicity was dose-dependent. Overdose leads to hypotension, bradycardia, arrhythmias, convulsions, respiratory depression, and potentially fetal distress if used in obstetrics. The major safety concern was the narrow therapeutic window and the risk of causing uterine tetany, which could compromise fetal oxygen supply. This contributed to its withdrawal from common clinical use.
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| References | |
| Additional Infomation |
(+)-Sparteine was once used clinically as a Class Ia antiarrhythmic agent and to induce or augment labor (as a uterine stimulant, paradoxically via ganglionic blockade in parasympathetic pathways). Due to safety concerns (particularly unpredictable pharmacokinetics and risk of fetal distress), its use has been largely discontinued in modern medicine. Today, it is primarily a research tool in autonomic pharmacology and an intermediate in alkaloid chemistry.
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| Molecular Formula |
C15H38N2O9S
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|---|---|
| Molecular Weight |
422.54
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| Related CAS # |
(+)-Sparteine;492-08-0
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| Appearance |
Off-white to brown solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~33.33 mg/mL (~78.88 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.92 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.92 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.92 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3666 mL | 11.8332 mL | 23.6664 mL | |
| 5 mM | 0.4733 mL | 2.3666 mL | 4.7333 mL | |
| 10 mM | 0.2367 mL | 1.1833 mL | 2.3666 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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